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21. 发明授权

US08058448B2 Processes and reagents for sulfurization of oligonucleotides 有权
标题翻译：寡核苷酸硫化的方法和试剂
公开(公告)号：US08058448B2
公开(公告)日：2011-11-15
申请号：US12351605
申请日：2009-01-09
申请人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
发明人： Muthiah Manoharan , Michael E. Jung , Kallanthottathil G. Rajeev , Rajendra K. Pandey , Gang Wang
IPC分类号： C07D285/01 , C07H21/00
CPC分类号： C07H21/00 , C07H21/04 , Y02P20/55
摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloramine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
摘要翻译：本发明涉及寡核苷酸合成和纯化的方法和试剂。本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。本发明的另一方面涉及硫转移剂。在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。在优选的实施方案中，色谱纯化是高效液相色谱法。

22. 发明授权

US5543510A Process and intermediates for the preparation of (+)-hydantocidin and analogs thereof 失效
标题翻译：制备（+） - 海马替丁及其类似物的方法和中间体
公开(公告)号：US5543510A
公开(公告)日：1996-08-06
申请号：US262411
申请日：1994-06-20
申请人： Philip M. Harrington , Michael E. Jung
发明人： Philip M. Harrington , Michael E. Jung
IPC分类号： C07D307/24 , A01N43/90 , C07D491/048 , C07D491/107 , C07H19/052 , C07H15/02
CPC分类号： C07H19/052
摘要： Hydantocidin is a potent non-selective herbicidal natural product. This invention provides an efficient method for the enantioselective preparation of (+)-hydantocidin, analogs thereof and intermediates therefor.
摘要翻译：海那氏苷是一种有效的非选择性除草天然产物。本发明提供了对映选择性制备（+） - 海马替丁，其类似物和其中间体的有效方法。

23. 发明授权

US5252538A (2-imidazolin-2-yl) fused heteropyridine compounds, intermediates for the preparation of and use of said compounds as herbicidal agents 失效
标题翻译：（2-咪唑啉-2-基）稠合的杂吡啶化合物，用于制备和使用所述化合物作为除草剂的中间体
公开(公告)号：US5252538A
公开(公告)日：1993-10-12
申请号：US465569
申请日：1990-01-16
申请人： Barrington Cross , Marinus Los , Robert F. Doehner, Jr. , David W. Ladner , Jerry L. Johnson , Michael E. Jung , Victor M. Kamhi , Shin-Shyong Tseng , John M. Finn , Peter J. Wepplo
发明人： Barrington Cross , Marinus Los , Robert F. Doehner, Jr. , David W. Ladner , Jerry L. Johnson , Michael E. Jung , Victor M. Kamhi , Shin-Shyong Tseng , John M. Finn , Peter J. Wepplo
IPC分类号： A01N43/90 , C07D401/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/10 , C07D491/14 , C07D491/147 , C07D495/04 , C07D497/04 , C07D498/04 , C07D498/22 , C07D513/04 , A01N43/36 , A01N43/40
CPC分类号： A01N43/90 , C07D401/04 , C07D471/04 , C07D491/04 , C07D491/10 , C07D491/14 , C07D495/04 , C07D497/04 , C07D513/04
摘要： There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
摘要翻译：提供了新颖的（2-咪唑啉-2-基）稠合的杂吡啶化合物和用于制备其的中间体化合物，以及用于控制多种多年生植物物种的方法。

24. 发明授权

US5220003A Process for the synthesis of 2',3'-dideoxynucleosides 失效
标题翻译：合成2'，3'-二脱氧核苷的方法
公开(公告)号：US5220003A
公开(公告)日：1993-06-15
申请号：US677500
申请日：1991-03-29
申请人： Michael E. Jung , John M. Gardiner
发明人： Michael E. Jung , John M. Gardiner
IPC分类号： C07D405/04 , C07D473/00 , C07H19/04 , C07H19/06
CPC分类号： C07D473/00 , C07D405/04 , C07H19/04 , C07H19/06
摘要： Methods are provided for preparing 3'-substituted-2',3'-dideoxynucleosides, and the like, from non-carbohydrate, non-nucleoside starting materials.
摘要翻译：提供从非碳水化合物，非核苷起始原料制备3'-取代-2'，3'-二脱氧核苷等的方法。

25. 发明申请

US20170226059A1 APOE4-TARGETED THERAPUTICS THAT INCREASE SIRT1 审中-公开
公开(公告)号：US20170226059A1
公开(公告)日：2017-08-10
申请号：US15500503
申请日：2015-08-19
申请人： Barbara JAGODZINSKA , Jesus CAMPAGNA , Johnny PHAM , Michael E. JUNG , Varghese JOHN , Rammohan RAO , Dale E. BREDESEN , The Regents of the University of California , Buck Institute for Research on Aging
发明人： Barbara Jagodzinska , Jesus Campagna , Johnny Pham , Michael E. Jung , Varghese John , Rammohan Rao , Dale E. Bredesen , Veena P. Theendakara
IPC分类号： C07D211/60 , C07D207/16 , C07C229/26 , C07C237/06 , C07C229/08 , C07C229/28
CPC分类号： C07D211/60 , A61K31/12 , A61K31/221 , A61P25/28 , C07C229/08 , C07C229/26 , C07C229/28 , C07C229/36 , C07C237/06 , C07C2601/04 , C07C2601/14 , C07D207/16
摘要： A link between ApoE4 allele and sirtuins expression level is identified that is believed to be associated with elevated risk for the promotion of processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway in a mammal leading to elevated risk for Alzheimer's disease. Compounds are identified that upregulate sirtuins (e.g., SirT1) expression levels and appear to be useful in the treatment and/or prophylaxis of MCI and/or Alzheimer's disease.

26. 发明授权

US09670244B2 Oxysterol compounds and the hedgehog pathway 有权
公开(公告)号：US09670244B2
公开(公告)日：2017-06-06
申请号：US12224430
申请日：2007-02-27
申请人： Farhad Parhami , Michael E. Jung , Jennifer R. Dwyer , Khanhlinh Nguyen
发明人： Farhad Parhami , Michael E. Jung , Jennifer R. Dwyer , Khanhlinh Nguyen
IPC分类号： A61K31/575 , C07J9/00
CPC分类号： C07J9/00
摘要： This invention relates, for example, to synthetic oxysterols. Also described are methods for using the compounds, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.

27. 发明授权

US09045474B2 Compounds and compositions for mitigating tissue damage and lethality 有权
标题翻译：用于减轻组织损伤和致死性的化合物和组合物
公开(公告)号：US09045474B2
公开(公告)日：2015-06-02
申请号：US13813923
申请日：2011-08-03
申请人： Robert H. Schiestl , Yelena O. Rivina , Michael E. Jung , Robert Damoiseaux
发明人： Robert H. Schiestl , Yelena O. Rivina , Michael E. Jung , Robert Damoiseaux
IPC分类号： C07D405/14 , A61K31/4704 , A61K31/4709 , A61P39/02 , C07D471/04 , A61K31/00 , A61K31/381 , A61K31/437 , G01N33/50 , A61K45/06 , A61N5/10 , C07D333/38 , C07D409/12 , C12Q1/02
CPC分类号： C07D471/04 , A61K31/00 , A61K31/381 , A61K31/437 , A61K31/4709 , A61K45/06 , A61N5/10 , C07D333/38 , C07D409/12 , C12Q1/025 , G01N33/5088 , G01N2800/40
摘要： Embodiments of the present invention provide compounds and compositions thereof, which are effective for mitigating tissue damage or lethality induced by an agent, and methods of making and using the same.
摘要翻译：本发明的实施方案提供了有效减轻由药剂引起的组织损伤或致死性的化合物及其组合物及其制备和使用方法。

28. 发明授权

US08883202B2 Lipid compositions 有权
标题翻译：脂质组合物
公开(公告)号：US08883202B2
公开(公告)日：2014-11-11
申请号：US13318600
申请日：2010-05-05
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Michael E. Jung
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Michael E. Jung
IPC分类号： A61K9/48 , A61K9/127 , A61K47/22
CPC分类号： A61K47/22 , A61K9/1272 , C07D295/13 , C12N15/113 , C12N15/1137 , C12N2310/14 , Y02A50/463
摘要： Disclosed herein are lipid compositions comprising a cationic lipid of formula (I), a neutral lipid, a sterol and a PEG or PEG-modified lipid, wherein formula (I) is (F). Also disclosed are methods of producing the cationic lipid of formula (I).
摘要翻译：本文公开了包含式（I）的阳离子脂质，中性脂质，固醇和PEG或PEG修饰的脂质的脂质组合物，其中式（I）是（F）。还公开了制备式（I）的阳离子脂质的方法。

29. 发明申请

US20130231518A1 COMPOUNDS AND COMPOSITIONS FOR MITIGATING TISSUE DAMAGE AND LETHALITY 有权
标题翻译：用于减轻组织损伤和损伤的化合物和组合物
公开(公告)号：US20130231518A1
公开(公告)日：2013-09-05
申请号：US13813923
申请日：2011-08-03
申请人： Robert H. Schiestl , Yelena O. Rivina , Michael E. Jung , Robert Damoiseaux
发明人： Robert H. Schiestl , Yelena O. Rivina , Michael E. Jung , Robert Damoiseaux
IPC分类号： C07D471/04 , C12Q1/02 , A61N5/10 , A61K31/381 , C07D409/12 , A61K45/06 , A61K31/437 , C07D333/38
CPC分类号： C07D471/04 , A61K31/00 , A61K31/381 , A61K31/437 , A61K31/4709 , A61K45/06 , A61N5/10 , C07D333/38 , C07D409/12 , C12Q1/025 , G01N33/5088 , G01N2800/40
摘要： Embodiments of the present invention provide compounds and compositions thereof, which are effective for mitigating tissue damage or lethality induced by an agent, and methods of making and using the same.
摘要翻译：本发明的实施方案提供了有效减轻由药剂引起的组织损伤或致死性的化合物及其组合物及其制备和使用方法。

30. 发明授权

US08445507B2 Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases 有权
标题翻译：雄激素受体调节剂用于治疗前列腺癌和雄激素受体相关疾病
公开(公告)号：US08445507B2
公开(公告)日：2013-05-21
申请号：US12294881
申请日：2007-03-27
申请人： Michael E. Jung , Charles L. Sawyers , Samedy Ouk , Chris Tran , John Wongvipat
发明人： Michael E. Jung , Charles L. Sawyers , Samedy Ouk , Chris Tran , John Wongvipat
IPC分类号： A61K31/4439 , C07D213/60
CPC分类号： A61K31/4439 , A61K9/48 , C07D401/04
摘要： A hydantoin compound useful for the prevention or treatment of hyperproliferative diseases or disorders.
摘要翻译：可用于预防或治疗过度增殖性疾病或障碍的乙内酰脲化合物。

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